Dabrafenib

Dabrafenib is an inhibitor of some mutated forms of BRAF kinases with in vitro IC 50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC 50 values of 3.2 and 5.0 nM, respectively, and other kinases, such as SIK1, NEK11, and LIMK1 at higher concentrations.

• TAFINLAR is a kinase inhibitor indicated as a single agent for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test. ( 1.1 , 2.1 ) TAFINLAR is indicated, in combination with trametinib , for: the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test.ICD-10: C43.9

• None. None.contraindicated

The recommended dosage of TAFINLAR in adult patients is 150 mg (two 75 mg capsules) orally twice daily. The recommended dosage for TAFINLAR in pediatric patients is based on body weight. Take TAFINLAR at least 1 hour before or 2 hours after a meal. ( 2 ) 2.1 Patient Selection Melanoma Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of treatment with TAFINLAR as a single agent [see Warnings and Precautions (5.2), Clinical Studies (14.1)] . Confirm the presence of BRAF V600E or V600K mutation in tumor specimens prior to initiation of treatment with TAFINLAR and trametinib [see Warnings and Precautions (5.2), Clinical Studies (14.2, 14.3)] . Information on FDA-approved tests for the detection of BRAF V600 mutations in melanoma is available at: http://www.fda.gov/CompanionDiagnostics . NSCLC Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of treatment with TAFINLAR and trametinib [see Clinical Studies (14.4)] . Information on FDA-approved tests for the detection of BRAF V600E mutations in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics . ATC Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of treatment with TAFINLAR and trametinib [see Clinical Studies (14.5)] . Information on FDA-approved tests for the detection of BRAF V600E mutations in ATC is available at: http://www.fda.gov/CompanionDiagnostics .

New Primary Malignancies, Cutaneous and Non-Cutaneous : Can occur when TAFINLAR is administered as a single agent or with trametinib. Monitor patients for new malignancies prior to, or while on therapy, and following discontinuation of treatment. ( 5.1 , 2.4 ) Tumor Promotion in BRAF Wild-type Tumors : Increased cell proliferation can occur with BRAF inhibitors. ( 5.2 , 2.1 ) Hemorrhage : Major hemorrhagic events can occur in patients receiving TAFINLAR with trametinib. Monitor for signs and symptoms of bleeding. ( 5.3 ) Cardiomyopathy : Assess left ventricular ejection fraction (LVEF) before treatment with TAFINLAR and trametinib, after one month of treatment, then every 2 to 3 months thereafter. ( 5.4 , 2.4 ) Uveitis : Perform ophthalmological evaluation for any visual disturbances. ( 5.5 , 2.4 ) Serious Febrile Reactions : Incidence and severity of pyrexia are increased with TAFINLAR and trametinib. ( 5.6 , 2.4 ) Serious Skin Toxicities : Monitor for skin toxicities. Discontinue for intolerable Grade 2 or for Grade 3 or 4 rash not improving within 3 weeks despite interruption of TAFINLAR. Permanently discontinue for severe cutaneous adverse reactions (SCARs). ( 5.7 , 2.4 ) Hyperglycemia : Monitor serum glucose levels in patients with preexisting diabetes or hyperglycemia. ( 5.8 ) Glucose-6-phosphate Dehydrogenase Deficiency (G6PD) : Closely monitor for hemolytic anemia. ( 5.9 ) Hemophagocytic Lymphohistiocytosis (HLH) : Interrupt treatment for suspected HLH. Discontinue treatment if HLH is confirmed. ( 5.11 ) Embryo-Fetal Toxicity : Can cause fetal harm.

The following clinically significant adverse reactions are described elsewhere in the labeling: New Primary Malignancies [see Warnings and Precautions (5.1)] Tumor Promotion in BRAF Wild-Type Tumors [see Warnings and Precautions (5.2)] Hemorrhage [see Warnings and Precautions (5.3)] Cardiomyopathy [see Warnings and Precautions (5.4)] Uveitis [see Warnings and Precautions (5.5)] Serious Febrile Reactions [see Warnings and Precautions (5.6)] Serious Skin Toxicities [see Warnings and Precautions (5.7)] Hyperglycemia [see Warnings and Precautions (5.8)] Glucose-6-Phosphate Dehydrogenase Deficiency [see Warnings and Precautions (5.9)] Hemophagocytic Lymphohistiocytosis [see Warnings and Precautions (5.11)] There are additional adverse reactions associated with trametinib. Refer to the trametinib prescribing information for additional information. Most common adverse reactions (≥ 20%) for TAFINLAR as a single agent are hyperkeratosis, headache, pyrexia, arthralgia, papilloma, alopecia, and palmar-plantar erythrodysesthesia syndrome. ( 6.1 ) Most common adverse reactions (≥ 20%) for TAFINLAR in combination with trametinib include: Unresectable or metastatic melanoma: pyrexia, rash, chills, headache, arthralgia, and cough. ( 6.1 ) Adjuvant treatment of melanoma: pyrexia, fatigue, nausea, headache, rash, chills, diarrhea, vomiting, arthralgia, and myalgia. ( 6.1 ) NSCLC: pyrexia, fatigue, nausea, vomiting, diarrhea, dry skin, decreased appetite, edema, rash, chills, hemorrhage, cough, and dyspnea.

Lactation : Do not breastfeed. ( 8.2 ) Females and Males of Reproductive Potential : May impair fertility. ( 8.3 ) 8.1 Pregnancy Risk Summary Based on findings from animal reproduction studies and its mechanism of action [see Clinical Pharmacology (12.1)] , TAFINLAR can cause fetal harm when administered to a pregnant woman. There is insufficient data in pregnant women exposed to TAFINLAR to assess the risks. Dabrafenib was teratogenic and embryotoxic in rats at doses three times greater than the human exposure at the recommended adult clinical dose of 150 mg twice daily (see Data) . Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In a combined female fertility and embryo-fetal development study in rats conducted during the period of organogenesis, developmental toxicity consisted of embryo-lethality, ventricular septal defects, and variation in thymic shape at a dabrafenib dose of 300 mg/kg/day [approximately three times the human exposure at the recommended adult dose based on area under the curve (AUC)].

Metabolism

Following administration of TAFINLAR capsules, dabrafenib C max and AUC increased in a dose-proportional manner across the dose range of 12 mg (0.08 times the approved recommended adult dose) to 300 mg (2 times the approved recommended adult dose), but the increase was less than dose-proportional after steady state twice-daily dosing. After twice-daily dosing, the mean accumulation ratio was 0.7, and the intersubject variability (CV%) of AUC at steady-state was 38%.

There is no information on overdosage of TAFINLAR. Since dabrafenib is highly bound to plasma proteins, hemodialysis is likely to be ineffective in the treatment of overdose with TAFINLAR.

• May 29, 2013NDANDA202806Novartis
• Mar 16, 2023NDANDA217514Novartis

1. 1Pyrexia4,04520%
2. 2Death2,86214%
3. 3Malignant Neoplasm Progression1,7378.4%
4. 4Fatigue1,4076.8%
5. 5Nausea1,3826.7%
6. 6Chills1,3146.4%
7. 7Rash1,1565.6%
8. 8Vomiting9714.7%
9. 9Diarrhoea9574.6%
10. 10Headache7373.6%
11. 11Asthenia7093.4%
12. 12Malaise6203.0%
13. 13Decreased Appetite5792.8%
14. 14Arthralgia5692.7%
15. 15Product Use In Unapproved Indication5322.6%

The 10 most recently updated of 189 ClinicalTrials.gov registrations naming Dabrafenib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Testing Trametinib and Dabrafenib as a Potential Targeted Treatment in Cancers With BRAF Genetic Changes (MATCH-Subprotocol H)
  Active not recruiting · Phase 2 · Interventional · 44 enrolled · National Cancer Institute (NCI)
  NCT04439292updated 2026-06-12
• Nivolumab With Trametinib and Dabrafenib, or Encorafenib and Binimetinib in Treating Patients With BRAF Mutated Metastatic or Unresectable Stage III-IV Melanoma
  Active not recruiting · Phase 2 · Interventional · 52 enrolled · M.D. Anderson Cancer Center
  NCT02910700updated 2026-06-11
• Pediatric Long-Term Follow-up and Rollover Study
  Active not recruiting · Phase 4 · Interventional · 165 enrolled · Novartis Pharmaceuticals
  NCT03975829updated 2026-06-11
• Dabrafenib and/or Trametinib Rollover Study
  Recruiting · Phase 4 · Interventional · 100 enrolled · Novartis Pharmaceuticals
  NCT03340506updated 2026-06-10
• Study of Efficacy and Safety of Dabrafenib in Combination With Trametinib in Previously Treated Patients With Metastatic, Radio-active Iodine Refractory BRAF V600E Mutation Positive Differentiated Thyroid Cancer
  Active not recruiting · Phase 3 · Interventional · 153 enrolled · Novartis Pharmaceuticals
  NCT04940052updated 2026-06-04
• Dabrafenib and Trametinib for BRAF V600 Mutant Low-Grade Gliomas
  Recruiting · Phase 2 · Interventional · 96 enrolled · University of California, San Francisco
  NCT07110246updated 2026-06-04
• Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
  Active not recruiting · Phase 2 · Interventional · 6,452 enrolled · National Cancer Institute (NCI)
  NCT02465060updated 2026-06-03
• Testing Dabrafenib and Trametinib With or Without Hydroxychloroquine in Stage IIIC or IV BRAF V600E/K Melanoma
  Terminated · Phase 2 · Interventional · 5 enrolled · ECOG-ACRIN Cancer Research Group
  NCT04527549updated 2026-06-01
• Dabrafenib and Trametinib Followed by Ipilimumab and Nivolumab or Ipilimumab and Nivolumab Followed by Dabrafenib and Trametinib in Treating Patients With Stage III-IV BRAFV600 Melanoma
  Active not recruiting · Phase 3 · Interventional · 267 enrolled · National Cancer Institute (NCI)
  NCT02224781updated 2026-05-29
• TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer
  Recruiting · Phase 2 · Interventional · 4,200 enrolled · American Society of Clinical Oncology
  NCT02693535updated 2026-05-29

CPIC-curated drug–gene pairs for Dabrafenib. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• G6PDCPIC CFDA label: Actionable PGx
  G6PD

Frequently asked questions

How does Dabrafenib work?

Dabrafenib is an inhibitor of some mutated forms of BRAF kinases with in vitro IC 50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC 50 values of 3.2 and 5.0 nM, respectively, and other kinases, such as SIK1, NEK11, and LIMK1 at higher concentrations.

What is Dabrafenib used for?

According to FDA labeling, Dabrafenib carries indications including: TAFINLAR is a kinase inhibitor indicated as a single agent for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test. ( 1.1 , 2.1 ) TAFINLAR is indicated, in combination with trametinib , for: the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Dabrafenib?

Dabrafenib is classified as B-Raf serine-threonine kinase (BRAF) inhibitors, Kinase Inhibitor, BRAF Serine/Threonine Kinase Inhibitors, Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 2B6 Inducers, Cytochrome P450 2C19 Inducers, Cytochrome P450 2C8 Inducers, Cytochrome P450 2C9 Inducers, Cytochrome P450 3A4 Inducers, Organic Anion Transporter 1 Inhibitors, Organic Anion Transporter 3 Inhibitors, Organic Anion Transporting Polypeptide 1B1 Inhibitors, Organic Anion Transporting Polypeptide 1B3 Inhibitors, Protein Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Dabrafenib?

Dabrafenib is marketed under brand names including Tafinlar.

What are the contraindications for Dabrafenib?

Dabrafenib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.